Lucitanib Inhibitor

Name: Lucitanib Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5754812
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5754812

Lucitanib (E-3810) is a novel dual VEGFR and FGFR inhibitor. It potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 (IC50s: 7nM, 25nM, 10nM, 17.5nM, and 82.5nM, respectively). More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

Lucitanib, Inhibitor

Full Product Name

Lucitanib

Product Synonym Names

E-3810

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

443.49

Solubility

DMSO: 25mg/mL (56.37mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C26H25N3O4

SMILES

O=C(NC)C1=CC=CC2=C1C=CC(OC3=CC=NC4=CC(OCC5(N)CC5)=C(OC)C=C43)=C2

CAS Number

1058137-23-7

Target & IC50

VEGFR1: ic50 7nM
VEGFR2: ic50 25nM
VEGFR3: ic50 10nM
FGFR1: ic50 17.5nM
FGFR2: ic50 82.5nM

In Vitro

Lucitanib, at oral dosing of 20mg/kg for 7 consecutive days, completely inhibits (P<0.01) the bFGF induced angiogenic response compare with the response in vehicle-treated mice. Lucitanib shows a broad spectrum of activity, being active in all the xenografts tested (HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas) with dose-dependent inhibition of tumor growthours. E-3810 significantly delays growth during treatment, but tumors resume their growth when treatment,is suspended; in a few cases, tumor regression is observed [1]. The activity of Lucitanib given at the doses of 15mg/kg is tested on MDA-MB-231 breast cancer transplanted subcutaneously, at a late stage, when tumor masses reach 350 to 400 mg. This tumor xenograft is very sensitive to Lucitanib, with complete tumor stabilization lasting throughout the 30-day treatment, As in other tumor models, tumors re-grow after the withdrawal of Lucitanib at a rate similar to control tumors [3].

Product Categories/Family for Lucitanib, inhibitor

Angiogenesis; VEGFR; Tyrosine Kinase/Adaptors

Product References and Citations for Lucitanib, inhibitor

Bello E, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
Bello E, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
Colzani M, et al. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509.
Colzani M, et al. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509.
Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with paclitaxel inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40
Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with paclitaxel inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40

Other Notes

Small volumes of Lucitanib, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Lucitanib purchase

MBS5754812 is an inhibitor targeting Lucitanib.